Акрипамид® ретард

General characteristics. Structure:

Active ingredient: 1,5 mg of an indapamid.

Excipients: лудипресс, gidroksipropilmetiltsellyuloz (gipromelloz), aerosil (silicon dioxide colloid), magnesium stearate, polyethyleneglycol (macrogoal), глицерол (glycerin), titanium dioxide, talc, lactose.

Pharmacological properties:

Pharmacodynamics. Anti-hypertensive means (diuretic, vazodilatator). On pharmacological properties it is close to thiazide diuretics (disturbance of a reabsorption of ions of sodium in a cortical segment of a Henle's loop). Increases allocation with urine of ions of sodium, chlorine and, to a lesser extent, potassium ions and magnesium. Having ability to selectively block "slow" calcium channels, increases elasticity of walls of arteries and reduces the general peripheric vascular resistance.

Promotes reduction of a hypertrophy of a left ventricle of heart. Does not influence lipidic and carbohydrate exchanges (including at patients with a diabetes mellitus), does not break sensitivity of peripheral fabrics to effect of insulin. Reduces sensitivity of a vascular wall to noradrenaline and angiotensin II, stimulates E2 prostaglandin synthesis, reduces products of free and stable oxygen radicals. The hypotensive effect develops by the end of the first week, remains during 24 h against the background of a single dose.

Pharmacokinetics. After intake it is quickly and completely soaked up from digestive tract; bioavailability — high (93%). Meal slows down absorption speed a little, but does not influence amount of the soaked-up substance. The maximum concentration in a blood plasma — 12 h after intake. At repeated methods of fluctuation of concentration of drug in a blood plasma in an interval between receptions of two doses decrease. Equilibrium concentration is established in 7 days of regular reception.

Elimination half-life — 18 h, communication with proteins of a blood plasma — 79%. Contacts also elastin of unstriated muscles of a vascular wall. Has the high volume of distribution, passes through gistogematichesky barriers (including placental), gets into breast milk. It is metabolized in a liver. Kidneys remove 60-80%, in the form of metabolites (in not changed look about 5% are removed), through intestines — 20%. At patients with a renal failure the pharmacokinetics does not change. Does not kumulirut.

Indications to use:

Arterial hypertension.

Route of administration and doses:

Inside, without chewing, washing down with enough liquid, preferential in the morning in a dose of 1,5 mg (1 tablet).

Features of use:

At the patients accepting cardiac glycosides, purgatives against the background of a giperaldostero-nizm, and also at elderly people regular control of maintenance of potassium ions and creatinine is shown.

Against the background of reception of an indapamid it is necessary to control systematically concentration of potassium ions, sodium, magnesium in a blood plasma (electrolytic disturbances can develop), рН, concentration of glucose, uric acid and residual nitrogen.

The most careful control is shown at patients with cirrhosis (especially with hypostases or ascites - risk of development of the metabolic alkalosis strengthening displays of hepatic encephalopathy), coronary heart disease, heart failure, and also at elderly people.

Patients with the increased QT interval on the electrocardiogram also treat group of the increased risk (inborn or developed against the background of any pathological process).

The first measurement of potassium concentration in blood should be taken within the first week of treatment.

The hypercalcemia against the background of reception of an indapamid can be a consequence of earlier not diagnosed hyperparathyreosis.

At patients with a diabetes mellitus it is extremely important to control glucose level in blood, especially in the presence of a hypopotassemia.

Considerable dehydration can lead to development of an acute renal failure (decrease in glomerular filtering). Patients need to offset loss of water and in an initiation of treatment carefully to control function of kidneys.

It is necessary for patients with arterial hypertension and a hyponatremia (owing to reception of diuretics) in 3 days prior to reception of inhibitors of an angiotensin-converting enzyme to stop reception of diuretics (if necessary reception of diuretics can be resumed a bit later), or by it appoint initial low doses of APF inhibitors.

Indapamid can yield a positive take when carrying out a drug test.

Influence on ability to drive the car and other mechanisms. The individual reactions connected with change of arterial pressure, especially in an initiation of treatment and at addition of other anti-hypertensive means are in certain cases possible. Therefore ability to driving and work with the mechanisms requiring special attention can decrease.

Side effects:

From the alimentary system: nausea, anorexia, dryness in a mouth, a gastralgia, vomiting, diarrhea, a lock, an abdominal pain, development of hepatic encephalopathy is possible, it is rare — pancreatitis.

From the central nervous system: adynamy, nervousness, headache, dizziness, drowsiness, вертиго, sleeplessness, depression; seldom — increased fatigue, the general weakness, an indisposition, a spasm of muscles, tension, irritability, alarm.

From respiratory system: cough, pharyngitis, sinusitis, it is rare — rhinitis.

From cardiovascular system: orthostatic hypotension, changes on the electrocardiogram (hypopotassemia), arrhythmia, heartbeat.

From an urinary system: frequent infections, nocturia, polyuria.

Allergic reactions: rash, urticaria, itch, hemorrhagic vasculitis.

Laboratory indicators: a hyperuricemia, a hyperglycemia, a hypopotassemia, a hypochloraemia, a hyponatremia, a hypercalcemia, increase in an urea nitrogen blood plasma, a giperkreatininemiya, a glucosuria.

Very seldom: thrombocytopenia, leukopenia, agranulocytosis, aplasia of marrow and hemolitic anemia.

Others: aggravation of a current of a system lupus erythematosus.

Interaction with other medicines:

Saluretics, cardiac glycosides, glyuko-and mineralokortikoida, тетракозактид, Amphotericinum In (in/in), purgatives increase risk of development of a hypopotassemia. At a concomitant use with cardiac glycosides the probability of development of digitalis intoxication increases; with calcium drugs — hypercalcemias; with Metforminum — aggravation of lactic acidosis is possible.

Increases concentration of ions of lithium in a blood plasma (decrease in removal with urine), lithium has nephrotoxic effect.

Astemizol, erythromycin in/in, pentamidine, сультоприд, терфенадин, Vincaminum, antiarrhytmic means of IA of a class (quinidine, Disopyramidum) and the III class (Amiodaronum, бретилиум, соталол) can lead to development of arrhythmia in the pirouette type (" torsades de pointes").

Non-steroidal anti-inflammatory drugs, glucocorticosteroid means, тетракозактид, sympathomimetics reduce hypotensive effect, Baclofenum — strengthens.

The combination with kaliysberegayushchy diuretics can be effective at some category of patients, however, at the same time the possibility of development hypo - or hyperpotassemias, especially at patients with a diabetes mellitus and a renal failure completely is not excluded.

Inhibitors of the angiotensin-converting enzyme (ACE) increase risk of development of arterial hypotension and/or acute renal failure (especially at the available renal artery stenosis).

Increases risk of development of renal failures when using iodinated contrast means in high doses (organism dehydration). Before use of iodinated contrast agents by the patient it is necessary to recover liquid loss.

Imipraminovy (tricyclic) antidepressants and neuroleptics strengthen hypotensive action and increase risk of development of orthostatic hypotension.

Cyclosporine increases risk of development of a giperkreatininemiya.

Reduces effect of indirect anticoagulants (derivative coumarin or an indandion) owing to increase in concentration of factors of coagulation as a result of reduction of volume of the circulating blood and increase in their products liver (dose adjustment can be required).

Strengthens the neuromuscular transmission blockade developing under the influence of not depolarizing muscle relaxants.

Contraindications:

Hypersensitivity to drug and other derivatives of sulfonamide, a heavy renal failure (an anury stage), a hypopotassemia, the expressed liver failure (including with encephalopathy), pregnancy, the lactation period, a concomitant use of the drugs extending QT interval, to patients with a lactose intolerance, a galactosemia, an absorption disturbance syndrome глюко-зы / galactoses, age to 18 years (efficiency and safety are not established).

With care appoint at abnormal liver functions and/or kidneys, disturbance of water and electrolytic balance, a hyperparathyreosis, the patient with the increased QT interval to an ECG or receiving the combined therapy, a diabetes mellitus in a stage of a decompensation, a hyperuricemia (especially, the followed gout and an uratny nephrolithiasis).

Overdose:

Symptoms: nausea, vomiting, weakness, dysfunction of digestive tract, water electro-литные disturbances, in certain cases — an excessive lowering of arterial pressure, respiratory depression. At patients with cirrhosis development of a hepatic coma is possible.

Treatment: gastric lavage, correction of water and electrolytic balance, symptomatic therapy. Specific antidote

Storage conditions:

List B. In the dry, protected from light place, at a temperature not above 25 °C. To store in the places unavailable to children. Not to use after the date specified on packaging. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

Tablets of the prolonged action, coated, on 1,5 mg. On 10 tablets in a blister strip packaging. 3 or 6 blister strip packagings together with the application instruction place in a pack from a cardboard.